title: Development of small-molecule inhibitors targeting adipose triglyceride lipase.
abstract: Adipose triglyceride lipase (ATGL) is rate limiting in the mobilization of fatty acids from cellular triglyceride stores. This central role in lipolysis marks ATGL as an interesting pharmacological target as deregulated fatty acid metabolism is closely linked to dyslipidemic and metabolic disorders. Here we report on the development and characterization of a small-molecule inhibitor of ATGL. Atglistatin is selective for ATGL and reduces fatty acid mobilization in vitro and in vivo.
authors.affiliation: Institute of Organic Chemistry, Graz University of Technology, 8010 Graz, Austria.
authors.forename: Nicole
authors.initials: N
authors.lastname: Mayer
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Martina
authors.initials: M
authors.lastname: Schweiger
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Matthias
authors.initials: M
authors.lastname: Romauch
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Gernot F
authors.initials: GF
authors.lastname: Grabner
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Thomas O
authors.initials: TO
authors.lastname: Eichmann
authors.affiliation: Institute of Organic Chemistry, Graz University of Technology, 8010 Graz, Austria.
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Fuchs
authors.affiliation: Institute of Organic Chemistry, Graz University of Technology, 8010 Graz, Austria.
authors.forename: Jakov
authors.initials: J
authors.lastname: Ivkovic
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Christoph
authors.initials: C
authors.lastname: Heier
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Irina
authors.initials: I
authors.lastname: Mrak
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Achim
authors.initials: A
authors.lastname: Lass
authors.affiliation: Institute of Pathology, Medical University of Graz, 8010 Graz, Austria.
authors.forename: Gerald
authors.initials: G
authors.lastname: Höfler
authors.affiliation: Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
authors.forename: Christian
authors.initials: C
authors.lastname: Fledelius
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Rudolf
authors.initials: R
authors.lastname: Zechner
authors.affiliation: Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
authors.forename: Robert
authors.initials: R
authors.lastname: Zimmermann
authors.affiliation: Institute of Organic Chemistry, Graz University of Technology, 8010 Graz, Austria.
authors.forename: Rolf
authors.initials: R
authors.lastname: Breinbauer
mesh_terms: D052436:Adipose Tissue, White; D000818:Animals; D015971:Gene Expression Regulation, Enzymologic; D020128:Inhibitory Concentration 50; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism*; D051379:Mice; D018345:Mice, Knockout; D015394:Molecular Structure; D010671:Phenylurea Compounds / Q000494:pharmacology*; D000217:Acyltransferases
chemical_list: D008049:Lipase; D010671:Phenylurea Compounds; C585749:atglistatin; C494445:PNPLA2 protein, mouse; D000217:Acyltransferases